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Mucoadhesive in situ gel formulation for vaginal delivery of clotrimazole: formulation, preparation, and in vitro/in vivo evaluation.

Authors :
Rençber, Seda
Karavana, Sinem Yaprak
Şenyiğit, Zeynep Ay
Eraç, Bayri
Limoncu, Mine Hoşgör
Baloğlu, Esra
Source :
Pharmaceutical Development & Technology; Jun2017, Vol. 22 Issue 4, p551-561, 11p
Publication Year :
2017

Abstract

The purpose of this study was to develop a suitable mucoadhesivein situgel formulation of clotrimazole (CLO) for the treatment of vaginal candidiasis. For this aim, the mixture of poloxamer (PLX) 407 and 188 were used to preparein situgels. Hydroxypropyl methylcellulose (HPMC) K100M or E50 was added toin situgels in 0.5% ratio to improve the mucoadhesive and mechanical properties of formulations and to prolong the residence time in vaginal cavity. After the preparation of mucoadhesivein situgels; gelation temperature/time, viscosity, mechanical, mucoadhesive, syringeability, spreadibility and rheological properties,in vitrorelease behavior, and anticandidal activities were determined. Moreover vaginal retention of mucoadhesivein situgels was investigated within vivodistribution studies in rats. Based on the obtained results, it was found that gels prepared with 20% PLX 407, 10% PLX 188 and 0.5% HPMC K100M/E50 might be suitable for vaginal administration of CLO. In addition, the results ofin vivodistribution studies showed that gel formulations remained on the vaginal mucosa even 24 h after application. In conclusion, the mucoadhesivein situgels of CLO would be alternative candidate for treatment of vaginal candidiasis since it has suitable gel properties with good vaginal retention. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
10837450
Volume :
22
Issue :
4
Database :
Complementary Index
Journal :
Pharmaceutical Development & Technology
Publication Type :
Academic Journal
Accession number :
122254120
Full Text :
https://doi.org/10.3109/10837450.2016.1163385